2. Protein Tyrosine Kinase/RTK Apoptosis
  3. c-Fms Apoptosis
  4. CSF1R-IN-22

CSF1R-IN-22 (Compound C19) is an orally effective CSF-1R selective inhibitor (IC50<6 nM). CSF1R-IN-22 enhances the secretion of CXCL9 from M2 macrophages, increases CD8+ T cell infiltration. CSF1R-IN-22 boosts anti-tumor immune responses of anti-PD-1, and induces apoptosis in tumor cells. CSF1R-IN-22 can effectively reprogram M2-like TAMs (tumor-associated macrophages) to the M1 phenotype and reshape the TME by inducing the recruitment of CD8+ T cells into tumors and reducing the infiltration of immunosuppressive Tregs and MDSCs.

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CSF1R-IN-22 Chemical Structure

CSF1R-IN-22 Chemical Structure

CAS No. : 2760585-35-9

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Description

CSF1R-IN-22 (Compound C19) is an orally effective CSF-1R selective inhibitor (IC50<6 nM). CSF1R-IN-22 enhances the secretion of CXCL9 from M2 macrophages, increases CD8+ T cell infiltration. CSF1R-IN-22 boosts anti-tumor immune responses of anti-PD-1, and induces apoptosis in tumor cells. CSF1R-IN-22 can effectively reprogram M2-like TAMs (tumor-associated macrophages) to the M1 phenotype and reshape the TME by inducing the recruitment of CD8+ T cells into tumors and reducing the infiltration of immunosuppressive Tregs and MDSCs[1].

In Vitro

CSF1R-IN-22 (0-2500 nM; 1 h) significantly inhibits the activation of CSF-1R signaling pathway in BMDMs cells[1].
CSF1R-IN-22 (30-100 nM; 24 h) efficiently reprograms M2-type macrophages to M1-type macrophages in BMDMs and HMDMs cells[1].
CSF1R-IN-22 (10-100 nM; 20 h) processed M2-type macrophage supernatants significantly inhibits MC-38 and CT-26 cell viability[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

CSF1R-IN-22 Related Antibodies

Western Blot Analysis[1]

Cell Line: BMDMs cells
Concentration: 10, 30, 100 nM
Incubation Time: 1 h
Result: Dose-dependently inhibited the phosphorylation of CSF-1R and its downstream signaling mediators AKT and mTORC1.

Apoptosis Analysis[1]

Cell Line: MC-38, CT-26 cells
Concentration: 10, 30, 100 nM
Incubation Time: 20 h
Result: Processed M2 macrophage supernatant significantly increased the apoptosis rate of MC-38 and CT-26 cells, with an increase of approximately 60% in the 100 nM concentration group.
In Vivo

CSF1R-IN-22 (10,20 mg/kg; p.o.; once daily for 14 days) shows significant antitumor activity and enhanced cytotoxic T-lymphocyte (CTLs) activity in C57BL/6 mice bearing subcutaneous MC-38 tumors, with the high-dose group exhibiting etter effect than PLX3397 (HY-16749)[1].
CSF1R-IN-22 (20 mg/kg; p.o.; once daily for 14 days) shows stronger anti-tumor effects when combined with 100 μg/mouse PD-1 antibody.CXCL9 expression is significantly positively correlated with survival[1].


Pharmacokinetic Analysis in SD rats[1]

Route Dose (mg/kg) AUC0-t (ng·h/mL) t1/2 (h) Cl (L/h/kg) Vss (L/kg) Cmax (ng/mL) F (%)
i.v. 1 9126.62 1.34 0.10 0.34 / /
p.o. 10 85 939.36 2.41 0.12 / 10 867.65 94.2

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: C57BL/6 mice bearing subcutaneous MC-38 tumors [1]
Dosage: 5,10,20 mg/kg
Administration: p.o.; once daily for 14 days
Result: Inhibited tumor growth, tumor mass was significantly lower than that of the control group, and induced apoptosis. In the high-dose group, tumor volume inhibition (TGI) was 65% and 30-day survival in mice was 70%.
Increased mRNA levels of M1 macrophage markers (Nos2, Tnf, Il6, Il1) and decreased expression of M2 macrophage markers (Arg1, Chil3l, Rentla, Mrc1).
(10 mg/kg and 20 mg/kg) Significantly increased the proportion of CD3+ CD8+ T cells. Dose-dependently reduced the proportion of immunosuppressive Treg cells and myeloid-derived suppressor cells (MDSCs) in tumor tissues.
Animal Model: C57BL/6 mice bearing subcutaneous MC-38 tumors or MC-38-luc [1]
Dosage: 20 mg/kg; 100 μg/mouse PD-1
Administration: p.o.; once daily for 14 days
Result: Significantly lower tumor bioluminescence intensity in the combination dose group than in the PD-1 antibody alone or C19 alone dose groups in both models.
The combination dose group significantly increased the proportion of CD3+ CD8+ T cells and CTLs in the tumor tissue while significantly decreasing the proportion of immunosuppressive Treg cells in the MC-38 tumor model. A significant increase in the infiltration of CD8+ T cells and CTLs correlated with a significant increase in the mRNA expression of Cxcl9.
Co-administered mice had 100% survival at 70 days, and 70% overcame tumor recurrence within 91 days after reinoculation with MC-38 tumor cells.
A significant reduction in apoptosis and a significant reduction in the proportion of CD3+ CD8+ T cells following the use of CXCL9-neutralizing antibody.
Molecular Weight

392.41

Formula

C20H20N6O3
CAS No.
Unlabeled CAS

SMILES

CC(C)(C1=CC(NC(NC2=CC(NC/3=O)=C(C=C2)C3=C\C4=CN=CN4)=O)=NO1)C
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Please store the product under the recommended conditions in the Certificate of Analysis.
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CSF1R-IN-22 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

CSF1R-IN-222760585-35-9c-FmsApoptosisCSF-1 receptorcolony stimulating factor 1 receptorCSF-1RCSF1RCXCL9 SecretionM2 Macrophage ReprogrammingT Cell InfiltrationAnti-Tumor Immune ResponseCancerImmune ModulationInhibitorinhibitorinhibit

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